| 产品描述: | TCJL37 is a potent, selective, and orally bioavailable TYK2 inhibitor with a Ki of 1.6 nM. TCJL37 can be used for the research of inflammatory bowel diseases (IBD) |
| 靶点: |
Tyk2:1.6 nM (Ki) |
| 体外研究: |
In cell-based assays, TCJL37 (Compound 37) shows IL-12 pSTAT4 EC50 of 224 nM. TCJL37 shows EC50s of 168 nM and 737 nM In human peripheral blood mononuclear cells (PBMC) and human whole blood assay, respectively |
| 体内研究: |
TCJL37 exhibits excellent oral exposure in CD-1 mice following oral administration (100 mg/kg). TCJL37 exhibits low clearance (1.0 mL/min/kg) in rat |
| 参考文献: |
1. Jun Liang, et al. Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors. J Med Chem. 2013 Jun 13;56(11):4521-36 |
| 溶解性: |
Soluble to 100 mM in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.654 ml |
13.272 ml |
26.543 ml |
| 5 mM |
0.531 ml |
2.654 ml |
5.309 ml |
| 10 mM |
0.265 ml |
1.327 ml |
2.654 ml |
| 50 mM |
0.053 ml |
0.265 ml |
0.531 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |